Solid Dispersions Incorporated into PVP Films for the Controlled Release of Trans-Resveratrol: Development, Physicochemical and In Vitro Characterizations and In Vivo Cutaneous Anti-Inflammatory Evaluation

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Riccio, Bruno Vincenzo Fiod ; do Nascimento, Andre Luiz Carneiro Soares ; Meneguin, Andreia Bagliotti ; Rodero, Camila Fernanda ; Santos, Kaio Pini ; Sabio, Rafael Miguel ; de Annunzio, Sarah Raquel ; Fontana, Carla Raquel ; Barud, Hernane da Silva ; Ferrari, Priscileila Colerato ; Chorilli, Marlus

• Document type: Journal article
• Source: PHARMACEUTICS; v. 14, n. 6, p. 21-pg., 2022-06-01.

Abstract

Trans-resveratrol can promote various dermatological effects. However, its high crystallinity decreases its solubility and bioavailability. Therefore, solid dispersions have been developed to promote its amorphization; even so, they present as powders, making cutaneous controlled drug delivery unfeasible and an alternative necessary for their incorporation into other systems. Thus, polyvinylpyrrolidone (PVP) films were chosen with the aim of developing a controlled delivery system to treat inflammation and bacterial infections associated with atopic dermatitis. Four formulations were developed: two with solid dispersions (and trans-resveratrol) and two as controls. The films presented with uniformity, as well as bioadhesive and good barrier properties. X-ray diffraction showed that trans-resveratrol did not recrystallize. Fourier-transform infrared spectroscopy (FT-IR) and thermal analysis evidenced good chemical compatibilities. The in vitro release assay showed release values from 82.27 +/- 2.60 to 92.81 +/- 2.50% (being a prolonged release). In the in vitro retention assay, trans-resveratrol was retained in the skin, over 24 h, from 42.88 to 53.28%. They also had low cytotoxicity over fibroblasts. The in vivo assay showed a reduction in inflammation up to 66%. The films also avoided Staphylococcus aureus's growth, which worsens atopic dermatitis. According to the results, the developed system is suitable for drug delivery and capable of simultaneously treating inflammation and infections related to atopic dermatitis. (AU)

• FAPESP's process: 19/19817-3 - Bioresponsive systems based on retrograded starch/pectin containing cellulose nanofibers as a strategy for 5-ASA colonic delivery in the treatment of Inflammatory Bowel Disease
• Grantee: Andréia Bagliotti Meneguin
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 18/09088-1 - Assessment of photodynamic therapy against polymicrobial acne biofilms: a preclinical study
• Grantee: Sarah Raquel de Annunzio
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 18/23015-7 - Antimicrobial photodynamic therapy by continuous and switched mode irradiation against Enterococcus faecalis and Cutibacterium acnes
• Grantee: Carla Raquel Fontana
• Support Opportunities: Regular Research Grants
• FAPESP's process: 18/25377-3 - Potential evaluation of cetuximab-modified mesoporous silica nanoparticles as docetaxel carrier to prostate cancer treatment.
• Grantee: Rafael Miguel Sábio
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 18/23357-5 - Multidrug co-crystals of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and Proton Pump Inhibitors (PPIs): development, characterization and biological evaluation in vitro and in vivo
• Grantee: André Luiz Carneiro Soares do Nascimento
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 19/00164-0 - Trans-resveratrol solid dispersions incorporated into polyvinylpyrrolidone membranes for cutaneous application: development, characterization and biological evaluation in vitro and in vivo
• Grantee: Bruno Vincenzo Fiod Riccio
• Support Opportunities: Scholarships in Brazil - Master